Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 86
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Pharmaceutics ; 13(9)2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34575403

RESUMO

Gastric cancer (GC) is a fatal malignant tumor, and effective therapies to attenuate its progression are lacking. Nanoparticle (NP)-based solutions may enable the design of novel treatments to eliminate GC. Refined, receptor-targetable NPs can selectively target cancer cells and improve the cellular uptake of drugs. To overcome the current limitations and enhance the therapeutic effects, epigallocatechin-3-gallate (EGCG) and low-concentration doxorubicin (DX) were encapsulated in fucoidan and d-alpha-tocopherylpoly (ethylene glycol) succinate-conjugated hyaluronic acid-based NPs for targeting P-selectin-and cluster of differentiation (CD)44-expressing gastric tumors. The EGCG/DX-loaded NPs bound to GC cells and released bioactive combination drugs, demonstrating better anti-cancer effects than the EGCG/DX combination solution. In vivo assays in an orthotopic gastric tumor mouse model showed that the EGCG/DX-loaded NPs significantly increased the activity of gastric tumors without inducing organ injury. Overall, our EGCG/DX-NP system exerted a beneficial effect on GC treatment and may facilitate the development of nanomedicine-based combination chemotherapy against GC in the future.

2.
Int J Mol Sci ; 22(10)2021 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-34069880

RESUMO

This research focuses on the proteolytic capacity of sea bass byproduct (SB) and their hypocholesterolemic activity via the cholesterol micelle formation (CMF) inhibition. SB was fermented with seven mixed lactic acid bacteria for 5 h at 42 °C. The lactic fermented SB was hydrolyzed with Protease N for 6 h under HHP to obtain the SB hydrolysates (HHP-assisted Protease N hydrolysis after fermentation, F-HHP-PN6). The supernatant was separated from the SB hydrolysate and freeze-dried. As the hydrolysis time extended to 6 h, soluble protein content increased from 187.1 to 565.8 mg/g, and peptide content increased from 112.8 to 421.9 mg/g, while inhibition of CMF increased from 75.0% to 88.4%. Decreasing the CMF inhibitory activity from 88.4% to 42.1% by simulated gastrointestinal digestion (FHHP-PN6 was further hydrolyzed by gastrointestinal enzymes, F-HHP-PN6-PP) reduced the CMF inhibitory activity of F-HHP-PN6. Using gel filtration chromatography, the F-HHP-PN6-PP was fractioned into six fractions. The molecular weight of the fifth fraction from F-HHP-PN6-PP was between 340 and 290 Da, and the highest inhibitory efficiency ratio (IER) on CMF was 238.9%/mg/mL. Further purification and identification of new peptides with CMF inhibitory activity presented the peptide sequences in Ser-Ala-Gln, Pro-Trp, and Val-Gly-Gly-Thr; the IERs were 361.7, 3230.0, and 302.9%/mg/mL, respectively.


Assuntos
Bass/metabolismo , Colesterol/química , Hidrolisados de Proteína/farmacologia , Sequência de Aminoácidos , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Anticolesterolemiantes/farmacologia , Antioxidantes/farmacologia , Fermentação , Hidrólise , Pressão Hidrostática , Micelas , Peso Molecular , Oligopeptídeos , Peptídeo Hidrolases/metabolismo , Peptídeos/química , Peptídeos/metabolismo , Hidrolisados de Proteína/metabolismo , Proteínas/química , Proteínas/metabolismo , Proteólise
3.
Opt Express ; 29(7): 10285-10306, 2021 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-33820168

RESUMO

This paper presents a passive autofocus algorithm applicable to interferometric microscopes. The proposed algorithm uses the number of slope variations in an image mask to locate the focal plane (based on focus-inflection points) and identify the two neighboring planes at which fringes respectively appear and disappear. In experiments involving a Mirau objective lens, the proposed algorithm matched the autofocusing performance of conventional algorithms, and significantly outperformed detection schemes based on zero-order interference fringe in dealing with all kinds of surface blemish, regardless of severity. In experiments, the proposed algorithm also proved highly effective in cases without fringes.

4.
Biomedicines ; 9(2)2021 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-33557143

RESUMO

Prostate cancer (PCa) is one of the most commonly diagnosed cancers in men and usually becomes refractory because of recurrence and metastasis. CD44, a transmembrane glycoprotein, serves as a receptor for hyaluronic acid (HA). It has been found to be abundantly expressed in cancer stem cells (CSCs) that often exhibit a radioresistant phenotype. Cytolethal distending toxin (CDT), produced by Campylobacter jejuni, is a tripartite genotoxin composed of CdtA, CdtB, and CdtC subunits. Among the three, CdtB acts as a type I deoxyribonuclease (DNase I), which creates DNA double-strand breaks (DSBs). Nanoparticles loaded with antitumor drugs and specific ligands that recognize cancerous cell receptors are promising methods to overcome the therapeutic challenges. In this study, HA-decorated nanoparticle-encapsulated CdtB (HA-CdtB-NPs) were prepared and their targeted therapeutic activity in radioresistant PCa cells was evaluated. Our results showed that HA-CdtB-NPs sensitized radioresistant PCa cells by enhancing DSB and causing G2/M cell-cycle arrest, without affecting the normal prostate epithelial cells. HA-CdtB-NPs possess maximum target specificity and delivery efficiency of CdtB into the nucleus and enhance the effect of radiation in radioresistant PCa cells. These findings demonstrate that HA-CdtB-NPs exert target specificity accompanied with radiomimetic activity and can be developed as an effective strategy against radioresistant PCa.

5.
Chemistry ; 27(12): 4176-4182, 2021 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-33244806

RESUMO

Daptomycin (DAP) is a calcium (Ca2+ )-dependent FDA-approved antibiotic drug for the treatment of Gram-positive infections. It possesses a complex pharmacophore hampering derivatization and/or synthesis of analogues. To mimic the Ca2+ -binding effect, we used a chemoenzymatic approach to modify the tryptophan (Trp) residue of DAP and synthesize kinetically characterized and structurally elucidated regiospecific Trp-modified DAP analogues. We demonstrated that the modified DAPs are several times more active than the parent molecule against antibiotic-susceptible and antibiotic-resistant Gram-positive bacteria. Strikingly, and in contrast to the parent molecule, the DAP derivatives do not rely on calcium or any additional elements for activity.


Assuntos
Daptomicina , Antibacterianos/farmacologia , Cálcio , Bactérias Gram-Positivas , Testes de Sensibilidade Microbiana
6.
Front Bioeng Biotechnol ; 8: 570490, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33042972

RESUMO

There is an increasing interest in the design of targeted carrier systems with combined therapeutic and diagnostic modalities. Therapeutic modalities targeting tumors with single ligand-based targeting nanocarriers are insufficient for proficient delivery and for targeting two different surface receptors that are overexpressed in cancer cells. Here, we evaluated an activated nanoparticle delivery system comprising fucoidan/hyaluronic acid to improve therapeutic efficacy. The system comprised polyethylene glycol-gelatin-encapsulated epigallocatechin gallate (EGCG), poly (D,L-lactide-co-glycolide; PLGA), and stable iron oxide nanoparticles (IOs). The latter enables targeting of prostate cancers in their molecular images. We demonstrate the transfer of nanoparticles and their entry into prostate cancer cells through ligand-specific recognition. This system may prove the benefits of drug delivery that enhances the inhibition of cell growth through apoptosis induction. Moreover, the improved targeting of nanotheranostics significantly suppressed orthotopic prostate tumor growth and more accurately targeted tumors compared with systemic combination therapy. In the presence of nanoparticles with iron oxides, the hypointensity of the prostate tumor was visualized on a T2-weignted magnetic resonance image. The diagnostic ability of this system was demonstrated by accumulating fluorescent nanoparticles in the prostate tumor from the in vivo imaging system, computed tomography. It is suggested that theranostic nanoparticles combined with a molecular imaging system can be a promising cancer therapy in the future.

7.
J Mater Chem B ; 8(45): 10416-10427, 2020 12 07.
Artigo em Inglês | MEDLINE | ID: mdl-33112350

RESUMO

Docetaxel-based chemotherapy for prostate cancer is the clinical standard of care. However, nonspecific targeting, multiple drug resistance, and adverse side effects are common obstacles. Various natural compounds, including epigallocatechin-3-gallate (EGCG) in combination with taxane, have the potential to be developed as anticancer therapeutics. Although synergistic hydrophobic-hydrophilic combination drugs have been used with some success, the main drawbacks of this approach are poor bioavailability, unfavorable pharmacokinetics, and low tissue distribution. To improve their synergistic effect and overcome limitations, we encapsulated EGCG and low-dose docetaxel within TPGS-conjugated hyaluronic acid and fucoidan-based nanoparticles. This approach might facilitate simultaneous target-specific markers at the edge and center of the tumor and then might increase intratumoral drug accumulation. Additionally, the successful release of bioactive combination drugs was regulated by the pH-sensitive nanoparticles and internalization into prostate cancer cells through CD44 and P-selectin ligand recognition, and the inhibition of cell growth via induced G2/M phase cell cycle arrest was observed in in vitro study. In in vivo studies, treatment with cancer-targeted combination drug-loaded nanoparticles significantly attenuated tumor growth and increased M30 protein expression without causing organ damage. Overall, the multifunctional nanoparticle system improved the drugs' synergistic effect, indicating great potential in its development as a prostate cancer treatment.


Assuntos
Antineoplásicos/administração & dosagem , Catequina/análogos & derivados , Docetaxel/administração & dosagem , Nanopartículas Multifuncionais/química , Neoplasias da Próstata/tratamento farmacológico , Microambiente Tumoral/efeitos dos fármacos , Animais , Antineoplásicos/uso terapêutico , Catequina/administração & dosagem , Catequina/uso terapêutico , Docetaxel/uso terapêutico , Portadores de Fármacos/química , Combinação de Medicamentos , Sistemas de Liberação de Medicamentos , Sinergismo Farmacológico , Humanos , Masculino , Camundongos SCID
8.
Int J Mol Sci ; 21(17)2020 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-32878305

RESUMO

The aim of this study was to develop a macrophage-targeted nanoparticle composed of hyaluronan/fucoidan complexes with polyethylene glycol-gelatin to encapsulate and deliver epigallocatechin-3-gallate (EGCG), a compound that can regulate macrophage activation and pro-inflammatory mediator production. We show that our nanoparticles can successfully bond to macrophages and deliver more EGCG than an EGCG solution treatment, confirming the anti-inflammatory effects of these nanoparticles in lipopolysaccharide-stimulated macrophages. The prepared nanoparticles were established with a small mean particle size (217.00 ± 14.00 nm), an acceptable polydispersity index (0.28 ± 0.07), an acceptable zeta potential value (-33.60 ± 1.30 mV), and a high EGCG loading efficiency (52.08% ± 5.37%). The targeting abilities of CD44 binding were increased as the hyaluronan concentration increased and decreased by adding a competitor CD44 antibody. Moreover, we found that fucoidan treatment significantly reduced macrophage migration after lipopolysaccharide treatment in a dose-responsive manner. In summary, we successfully created macrophage-targeted nanoparticles for effective targeted delivery of EGCG, which should aid in the development of future anti-inflammatory drugs against macrophage-related diseases.


Assuntos
Catequina/análogos & derivados , Sistemas de Liberação de Medicamentos , Ácido Hialurônico/química , Inflamação/tratamento farmacológico , Macrófagos/efeitos dos fármacos , Nanopartículas/administração & dosagem , Polissacarídeos/química , Animais , Catequina/química , Catequina/farmacologia , Movimento Celular , Portadores de Fármacos/química , Receptores de Hialuronatos/metabolismo , Inflamação/induzido quimicamente , Lipopolissacarídeos , Macrófagos/metabolismo , Camundongos , Nanopartículas/química , Células RAW 264.7
9.
Polymers (Basel) ; 12(5)2020 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-32456005

RESUMO

This study focuses on preparation and valuation of the biodegradable, native, and modified gelatin film as screen-printing substrates. Modified gelatin film was prepared by crosslinking with various crosslinking agents and the electrode array was designed by screen-printing. It was observed that the swelling ratio of C-2, crosslinked with glutaraldehyde and EDC/NHS (1-ethyl-3-(3-dimethylaminopropyl) carbodiimide/N-hydroxysuccinimide) was found to be lower (3.98%) than that of C-1 (crosslinked with only glutaraldehyde) (8.77%) and C-0 (without crosslinking) (28.15%). The obtained results indicate that the swelling ratios of both C-1 and C-2 were found to be lower than that of C-0 (control one without crosslinking). The Young's modulus for C-1 and C-2 was found to be 8.55 ± 0.57 and 23.72 ± 2.04 kPa, respectively. Hence, it was conveyed that the mechanical strength of C-2 was found to be two times higher than that of C-l, suggesting that the mechanical strength was enhanced upon dual crosslinking in this study also. The adhesion study indicates that silver ink adhesion on the gelation surface is better than that of carbon ink. In addition, the electrical response of C-2 with a screen-printed electrode (SPE) was found to be the same as the commercial polycarbonate (PC) substrate. The result of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay suggested that the silver SPE on C-2 was non-cytotoxic toward L929 fibroblast cells proliferation. The results indicated that C-2 gelatin is a promising material to act as a screen-printing substrate with excellent biodegradable and biocompatible properties.

11.
J Nanobiotechnology ; 18(1): 58, 2020 Apr 09.
Artigo em Inglês | MEDLINE | ID: mdl-32272948

RESUMO

BACKGROUND: The anti-angiogenic fusion protein RBDV-IgG1 Fc (RBDV), which comprises the receptor-binding domain of vascular endothelial growth factor-A (VEGF-A), has shown antitumour effects by reducing angiogenesis in vivo. This study used the cationic lipoplex lipo-PEG-PEI-complex (LPPC) to simultaneously encapsulate both the RBDV targeting protein and the RBDV plasmid (pRBDV) without covalent bonds to assess VEGFR targeting gene therapy in mice with melanoma in vivo. RESULTS: LPPC protected the therapeutic transgene from degradation by DNase, and the LPPC/RBDV complexes could specifically target VEGFR-positive B16-F10 cells both in vitro and in vivo. With or without RBDV protein-targeting direction, the pRBDV-expressing RBDV proteins were expressed and reached a maximal concentration on the 7th day in the sera after transfection in vivo and significantly elicited growth suppression against B16-F10 melanoma but not IgG1 control proteins. In particular, LPPC/pRBDV/RBDV treatment with the targeting molecules dramatically inhibited B16-F10 tumour growth in vivo to provide better therapeutic efficacy than the treatments with gene therapy with IgG1 protein targeting or administration of a protein drug with RBDV. CONCLUSIONS: The simultaneous combination of the LPPC complex with pRBDV gene therapy and RBDV protein targeting might be a potential tool to conveniently administer targeted gene therapy for cancer therapy.


Assuntos
Inibidores da Angiogênese/genética , Terapia Genética/métodos , Lipossomos/química , Melanoma Experimental/terapia , Receptores de Fatores de Crescimento do Endotélio Vascular/metabolismo , Células 3T3 , Animais , Linhagem Celular Tumoral , Proliferação de Células , Fragmentos Fc das Imunoglobulinas/genética , Fragmentos Fc das Imunoglobulinas/metabolismo , Masculino , Melanoma Experimental/mortalidade , Melanoma Experimental/patologia , Camundongos , Camundongos Endogâmicos C57BL , Plasmídeos/química , Plasmídeos/genética , Plasmídeos/uso terapêutico , Domínios Proteicos/genética , Receptores de Fatores de Crescimento do Endotélio Vascular/genética , Proteínas Recombinantes de Fusão/biossíntese , Proteínas Recombinantes de Fusão/isolamento & purificação , Taxa de Sobrevida , Transplante Homólogo , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo
12.
ACS Appl Mater Interfaces ; 11(27): 23880-23892, 2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31192580

RESUMO

Various natural compounds including epigallocatechin gallate (EGCG) and curcumin (CU) have potential in developing anticancer therapy. However, their clinical use is commonly limited by instability and low tissue distribution. EGCG and CU combined treatment can improve the efficacy with synergistic effects. To improve the synergistic effect and overcome the limitations of low tissue distribution, we applied a dual cancer-targeted nanoparticle system to co-deliver EGCG and CU. Nanoparticles were composed of hyaluronic acid, fucoidan, and poly(ethylene glycol)-gelatin to encapsulate EGCG and CU. Furthermore, a dual targeting system was established with hyaluronic acid and fucoidan, which were used as agents for targeting CD44 on prostate cancer cells and P-selectin in tumor vasculature, respectively. Their effect and efficacy were investigated in prostate cancer cells and a orthotopic prostate tumor model. The EGCG/CU-loaded nanoparticles bound to prostate cancer cells, which were uptaken more into cells, leading to a better anticancer efficiency compared to the EGCG/CU combination solution. In addition, the releases of EGCG and CU were regulated by their pH value that avoided the premature release. In mice, treatment of the cancer-targeted EGCG/CU-loaded nanoparticles significantly attenuated the orthotopic tumor growth without inducing organ injuries. Overall, the dual-targeted nanoparticle system for the co-delivery of EGCG and CU greatly improved its synergistic effect in cancer therapy, indicating its great potential in developing treatments for prostate cancer therapy.


Assuntos
Catequina/análogos & derivados , Curcumina , Sistemas de Liberação de Medicamentos , Neoplasias Experimentais/tratamento farmacológico , Neoplasias da Próstata/tratamento farmacológico , Animais , Catequina/química , Catequina/farmacocinética , Catequina/farmacologia , Curcumina/farmacocinética , Curcumina/farmacologia , Humanos , Receptores de Hialuronatos/metabolismo , Masculino , Camundongos , Camundongos SCID , Proteínas de Neoplasias/metabolismo , Neoplasias Experimentais/diagnóstico por imagem , Neoplasias Experimentais/metabolismo , Selectina-P/metabolismo , Células PC-3 , Neoplasias da Próstata/diagnóstico por imagem , Neoplasias da Próstata/metabolismo , Ensaios Antitumorais Modelo de Xenoenxerto
13.
Nutrients ; 11(6)2019 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-31208053

RESUMO

This research focuses on cobia skin hydrolysates and their antihypertensive effects via the inhibitory activities of angiotensin I-converting enzyme (ACE). Marine fish Cobia (Rachycentron canadum) skin was hydrolysed for 5 h using Protamex and Protease N to obtain the cobia skin protein hydrolysates PX-5 and PN-5, respectively. The soluble protein and peptide contents of the PX-5 were 612 and 270 mg/g, respectively, and for the PN-5, 531 and 400 mg/g, respectively. The IC50 of PX-5 and PN-5 on ACE was 0.221 and 0.291 mg/mL, respectively. Increasing the IC50 from 0.221 to 0.044 mg/mL by simulated gastrointestinal digestion (PX-5G) reduced the ACE-inhibitory capacity of PX-5. Using gel filtration chromatography, the PX-5G was fractioned into eight fractions. The molecular weight of the fifth fraction from PX-5G was between 630 and 450 Da, and the highest inhibitory efficiency ratio on ACE was 1552.4%/mg/mL. We identified four peptide sequences: Trp-Ala-Ala, Ala-Trp-Trp, Ile-Trp-Trp, and Trp-Leu, with IC50 values for ACE of 118.50, 9.40, 0.51, and 26.80 µM, respectively. At a dose of 600 mg PX-5 powder/kg body weight, in spontaneously hypertensive rats PX-5's antihypertensive effect significantly reduced systolic and diastolic blood pressure by 21.9 and 15.5 mm Hg, respectively, after 4 h of oral gavage.


Assuntos
Anti-Hipertensivos/farmacologia , Peixes , Peptídeos/farmacologia , Hidrolisados de Proteína/farmacologia , Pele/química , Sequência de Aminoácidos , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Cromatografia em Gel , Digestão , Hipertensão/tratamento farmacológico , Peso Molecular , Ratos , Ratos Endogâmicos SHR
14.
Virology ; 533: 125-136, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-31153047

RESUMO

There is still limited information on the diversity of (-)ssRNA viruses that infect fungi. Here, we have discovered two novel (-)ssRNA mycoviruses in the shiitake mushroom (Lentinula edodes). The first virus has a monopartite RNA genome and relates to that of mymonaviruses (Mononegavirales), especially to Hubei rhabdo-like virus 4 from arthropods and thus designated as Lentinula edodes negative-strand RNA virus 1. The second virus has a putative bipartite RNA genome and is related to the recently discovered bipartite or tripartite phenui-like viruses (Bunyavirales) associated with plants and ticks, and designated as Lentinula edodes negative-strand RNA virus 2 (LeNSRV2). LeNSRV2 is likely the first segmented (-)ssRNA virus known to infect fungi. Its smaller RNA segment encodes a putative nucleocapsid and a plant MP-like protein using a potential ambisense coding strategy. These findings enhance our understanding of the diversity, evolution and spread of (-)ssRNA viruses in fungi.


Assuntos
Micovírus/isolamento & purificação , Vírus de RNA/isolamento & purificação , Cogumelos Shiitake/virologia , Sequência de Bases , Micovírus/genética , Filogenia , Vírus de RNA/classificação , Vírus de RNA/genética , RNA Viral/genética
15.
J Clin Med ; 8(1)2019 Jan 14.
Artigo em Inglês | MEDLINE | ID: mdl-30646625

RESUMO

The bacterial species, Helicobacter pylori, is associated with several gastrointestinal diseases, and poses serious health threats owing to its resistance to antibiotics. Lactobacillus spp., on the other hand, possess probiotic activities that have beneficial effects in humans. However, the mechanisms by which Lactobacillus spp. harbor favorable functions and act against H. pylori infection remain to be explored. The aim of this study was to investigate the ability of bacterial strains, Lactobacillus rhamnosus and Lactobacillus acidophilus, termed GMNL-74 and GMNL-185, respectively, to inhibit H. pylori growth and inflammation. Our results showed that GMNL-74 and GMNL-185 possess potent antimicrobial activity against multidrug resistant (MDR)-H. pylori. In addition, an in vitro cell-based model revealed that the inhibition of H. pylori adhesion and invasion of gastric epithelial cells and interleukin-8 production were significantly decreased by treatment with both the Lactobacillus strains. In vivo studies demonstrated that colonization of H. pylori and induced inflammation in the mouse stomach were also alleviated by these Lactobacillus strains. Furthermore, the abundance of beneficial gut bacteria, including Bifidobacterium spp. and Akkermansia muciniphilia, were significantly increased in H. pylori-infected mice treated with GMNL-74 and GMNL-185. These results demonstrate that Lactobacillus spp. ameliorate H. pylori-induced inflammation and supports beneficial gut specific bacteria that act against H. pylori infection.

16.
Nutrients ; 10(10)2018 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-30275420

RESUMO

Hot water was used to obtain Chlorella sorokiniana hot water extract (HWE). Subsequently, this byproduct was freeze-dried, hydrolysed at 50 °C using Protease N to obtain C. sorokiniana protein hydrolysates (PN-1), and then digested with a gastrointestinal enzyme (PN-1G). The inhibitory effects of the HWE and hydrolysates against angiotensin I-converting enzyme (ACE) were investigated. The soluble protein and peptide contents were 379.9 and 179.7 mg/g, respectively, for HWE and 574.8 and 332.8 mg/g, respectively, for PN-1. The IC50 values of the HWE, PN-1, and PN-1G on ACE were 1.070, 0.035, and 0.044 mg/mL, respectively. PN-1G was separated into seven fractions through size exclusion chromatography. The sixth fraction of the hydrolysate had a molecular weight between 270 and 340 Da, and the lowest IC50 value on ACE was 0.015 mg/mL. The amino acid sequences of the ACE-inhibitory peptides were Trp-Val, Val-Trp, Ile-Trp, and Leu-Trp, of which the IC50 values were 307.61, 0.58, 0.50, and 1.11 µΜ, respectively. Systolic blood pressure and diastolic blood pressure were reduced 20 and 21 mm Hg, respectively, in spontaneously hypertensive rats after 6 h of oral administration with a dose of 171.4 mg PN-1 powder/kg body weight.


Assuntos
Inibidores da Enzima Conversora de Angiotensina/farmacologia , Anti-Hipertensivos/farmacologia , Chlorella/química , Peptídeos/farmacologia , Hidrolisados de Proteína/farmacologia , Sequência de Aminoácidos , Animais , Pressão Sanguínea/efeitos dos fármacos , Cromatografia em Gel , Hipertensão/tratamento farmacológico , Masculino , Peso Molecular , Ratos , Ratos Endogâmicos SHR
17.
Molecules ; 23(4)2018 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-29642399

RESUMO

This study utilized pomelo steam distillation to isolate pomelo peel essential oil. The constituents were then analyzed through gas chromatography-mass spectrometry (GC-MS), and the antibacterial activity of the essential oil emulsions at different homogenizer speed conditions and concentrations of water-soluble chitosan (degree of acetylation, DA = 54.8%) against S. aureus and E. coli was examined. Analysis of the essential oil composition identified a total of 33 compounds with the main constituent, limonene accounting for 87.5% (940.07 mg/g) of the total. The pomelo peel oil was emulsified through homogenization at 24,000 rpm, resulting in a minimal inhibitory concentration (MIC) for E. coli that was 1.9 times lower than that of the essential oil without homogenization. In addition, a mixture of 0.4% essential oil emulsion and 0.03% water-soluble chitosan had the strongest synergetic antibacterial effect on S. aureus and E. coli at pH 7.4. In comparison with chitosan alone, the MIC value of this mixture was significantly 2.4 and 2.5 times lower. Hence, this study suggests using a mixture of emulsified pomelo peel oil and water-soluble chitosan to develop a novel natural food preservative, and that the processability of food, as well as the economic value of the byproducts of the Taiwan Matou pomelo and chitosan, could be increased.


Assuntos
Antibacterianos/farmacologia , Quitosana/farmacologia , Citrus/química , Óleos Voláteis/farmacologia , Antibacterianos/química , Quitosana/química , Cicloexenos/isolamento & purificação , Cicloexenos/farmacologia , Escherichia coli/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Limoneno , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Vegetais/química , Óleos Vegetais/farmacologia , Solubilidade , Staphylococcus aureus/efeitos dos fármacos , Terpenos/isolamento & purificação , Terpenos/farmacologia
18.
ACS Appl Mater Interfaces ; 10(31): 25866-25870, 2018 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-29481039

RESUMO

This study introduces a cyclical annealing technique that enhances the reliability of amorphous indium-gallium-zinc-oxide (a-IGZO) via-type structure thin film transistors (TFTs). By utilizing this treatment, negative gate-bias illumination stress (NBIS)-induced instabilities can be effectively alleviated. The cyclical annealing provides several cooling steps, which are exothermic processes that can form stronger ionic bonds. An additional advantage is that the total annealing time is much shorter than when using conventional long-term annealing. With the use of cyclical annealing, the reliability of the a-IGZO can be effectively optimized, and the shorter process time can increase fabrication efficiency.

19.
ACS Biomater Sci Eng ; 4(8): 2847-2859, 2018 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-33435008

RESUMO

The clinical treatment of gastric cancer is hampered by the development of anticancer drug resistance as well as the unfavorable pharmacokinetics, nontarget toxicity, and inadequate intratumoral accumulation of current chemotherapies. The polyphenol epigallocatechin gallate in combination with doxorubicin exhibits synergistic inhibition P-glycoprotein efflux pump activity and cancer cell growth. This study evaluated a potential activated nanoparticle delivery system comprising a hyaluronic acid complex with polyethylene glycol-conjugated gelatin containing encapsulated epigallocatechin gallate and low-dose doxorubicin, which may facilitate targeted drug administration to gastric cancer cells. We confirmed successful delivery of bioactive combination drugs and internalization into gastric cancer cells through CD44 ligand recognition and ensuing inhibition of cell proliferation via caspase-induced apoptosis and G2/M phase cell cycle arrest. Furthermore, the targeted nanoparticles significantly suppressed gastric tumor activity and reduced both tumor and heart tissue inflammatory reaction in vivo compared to systemic combination treatment.

20.
Front Microbiol ; 8: 692, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28484439

RESUMO

Influenza A virus PB1-F2, encoding a multi-functional protein, is regarded as a virulent gene. Variation in expression pattern and protein stability among PB1-F2 proteins derived from different strains may explain why PB1-F2 functions in a strain- and cell type-specific manner. Because the protein stability of PB1-F2 affects its biological functions, we looked for sequences important for this property. By comparing variants and chimeric of PB1-F2 proteins from A/Hong Kong/156/1997 (H5N1) and A/Puerto Rico/8/1934 (H1N1), we identified amino acid residues 68-71 affect its protein stability. PB1-F2 with T68, Q69, D70, and S71 has a shorter protein half-life than its I68, L69, V70, and F71 counterpart. This is likely to do with proteasome-mediated degradation. Swapping amino acids 68-71 between two proteins reversed not only the length of protein half-life and sensitivity to MG132, but also subcellular localization and interferon antagonization. Our data suggested that composition of amino acids 68-71, which regulates protein stability and therefore its functions, can be a major factor determining strain-specificity of PB1-F2.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...